Oxycodone, Naloxone

Products

The fixed combination Targin with the active ingredients oxycodone and naloxone was approved in many countries in 2009. In other countries, the drug is also known as Targinact or Targiniq. In 2016, generic versions were approved in many countries. They went on sale in 2018.

Structure and properties

Oxycodone (C18H21NO4, Mr = 315.4 g/mol) and naloxone (C19H21NO4, Mr = 327.37 g/mol) are present in the drug as oxycodone and naloxone hydrochloride, respectively.

Effects

Oxycodone (ATC N02AA55) is a semisynthetic opioid with analgesic and depressant properties. Naloxone (ATC V03AB15) is a competitive opioid antagonist at all opioid receptors that abolishes the effects of oxycodone locally in the intestine, thereby counteracting the development of constipation. Naloxone has a low bioavailability of about two percent due to high first-pass metabolism and therefore acts locally in the gut without central effects. It must therefore be administered parenterally to treat opioid poisoning.

Indications

For the treatment of pain.

Dosage

According to the SmPC. The sustained-release tablets are taken in the morning and evening (every 12 hours) and independently of meals.

Contraindications

Numerous precautions must be observed when using opioids. Full details can be found in the drug label.

Adverse effects

The most common possible adverse effects include: